A-286501
A-286501 is an orally active adenosine kinase inhibitor with an IC50 of 0.47 nM (rat brain cytosol). A-286501 blocks the phosphorylation of adenosine to AMP and increases adenosine. A-286501 mediates non-opioid adenosine receptor-dependent antinociceptive and anti-inflammatory effects, reduces paw edema, myeloperoxidase activity, and tactile allodynia, and produces antinociceptive effects in acute, inflammatory, neuropathic, and hyperalgesic models. A-286501 can be used in research on inflammatory pain, neuropathic pain, and diabetic neuropathy.
For research use only. We do not sell to patients.
- CAS No.: 483341-15-7
- Formula: C11H14BrN5O2
- Molecular Weight:328.17
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| IMR-32 | IC50 |
11.6 nM
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Inhibition of adenosine kinase (AK) activity in intact cultured human IMR-32 neuroblastoma cells.
Inhibition of adenosine kinase (AK) activity in intact cultured human IMR-32 neuroblastoma cells.
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11932067 |
In Vitro
A-286501 is a potent AK inhibitor across mammalian species and recombinant human AK subtypes, with an IC50 of 0.47 nM against rat brain cytosolic AK and IC50 values of 0.6-4.6 nM across the tested species/subtypes[1].
A-286501 (100 nM; 18 h) is a reversible AK inhibitor that exhibits competitive inhibition with respect to Adenosine (ADO) (HY-B0228) (Ki = 1.87 nM) and noncompetitive inhibition with respect to MgATP2− (Ki = 8.86 nM) when using rat brain cytosolic AK and human recombinant AK[1].
A-286501 exhibits much higher selectivity for AK than for ADO receptors, ADO transporters, ADO deaminase, P2 receptors, and a broad 86-target panel, with IC50 values greater than 100 μM at ADO-related sites and IC50 values greater than 10 μM in the Cerep panel[1].
A-286501 inhibits ADO phosphorylation in intact IMR-32 human neuroblastoma cells with an IC50 of 11.6 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 483341-15-7
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Molecular Weight 328.17
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Formula C11H14BrN5O2
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SMILES
O[C@H]1[C@@H](C[C@@H]([C@H]1O)N)N2C3=NC=NC(N)=C3C(Br)=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
A-286501 Related Classifications
HY-116005 Related Classifications
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